ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : -64 مورد

Butorphanol: Drug information

Butorphanol: Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Butorphanol: Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Addiction, abuse, and misuse:

Because the use of butorphanol exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death, assess each patient's risk prior to prescribing and reassess all patients regularly for the development of these behaviors and conditions.

Opioid analgesic risk evaluation and mitigation strategy (REMS) (intranasal):

Health care providers are strongly encouraged to complete a REMS-compliant education program and to counsel patients and caregivers on serious risk, safe use, and the importance of reading the Medication Guide with each prescription.

Life-threatening respiratory depression:

Serious, life-threatening, or fatal respiratory depression may occur with use of butorphanol, especially during initiation or following a dose increase. To reduce the risk for respiratory depression, proper dosing and titration of butorphanol are essential.

Accidental exposure (intranasal):

Accidental exposure of even one dose of butorphanol, especially by children, can result in a fatal overdose of butorphanol.

Neonatal opioid withdrawal syndrome:

If opioid use is required for an extended period of time in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome (NOWS), which may be life-threatening if not recognized and treated. Ensure that management by neonatology experts will be available at delivery.

Risk from concomitant use with benzodiazepines or other CNS depressants:

Concomitant use of opioids with benzodiazepines or other CNS depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of butorphanol and benzodiazepines or other CNS depressants for use in patients for whom alternative treatment options are inadequate.

CYP3A4 interaction (intranasal):

The concomitant use of butorphanol with all CYP3A4 inhibitors may result in an increase in butorphanol plasma concentrations, which could increase or prolong adverse reactions and may cause potentially fatal respiratory depression. In addition, discontinuation of a concomitantly used CYP3A4 inducer may result in an increase in butorphanol plasma concentration. Monitor patients receiving butorphanol and any CYP3A4 inhibitor or inducer.

Pharmacologic Category
  • Analgesic, Opioid;
  • Analgesic, Opioid Partial Agonist
Dosing: Adult

Dosage guidance:

Safety: Consider prescribing naloxone or nalmefene for patients with factors associated with an increased risk for overdose, such as history of overdose or substance use disorder, patients with sleep-disordered breathing, higher opioid dosages (≥50 morphine milligram equivalents [MME]/day orally), and/or concomitant benzodiazepine use (Ref).

Dosing: Dosing provided is based on typical doses; some patients may require higher or lower doses. Individualize dosing based on patient-specific factors (eg, severity of pain, comorbidities, degree of opioid experience/tolerance) and titrate to patient-specific treatment goals (eg, improvement in function and quality of life, decrease in pain using a validated pain rating scale). Use the lowest effective dose for the shortest period of time.

Clinical considerations: Opioids may be part of a comprehensive, multimodal, patient-specific treatment plan for managing moderate to severe pain. Maximize nonopioid analgesia (when appropriate) prior to initiation of opioid analgesia. Reserve butorphanol for patients for whom alternative treatment options (eg, nonopioid analgesics, opioid combination products) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. Butorphanol has an analgesic ceiling (Ref).

Acute pain

Acute pain (alternative agent):

IM: Initial: 2 mg in patients who will be able to remain recumbent (in the event drowsiness or dizziness occurs); may repeat every 3 to 4 hours as needed; usual range: 1 to 4 mg every 3 to 4 hours as needed.

IV: Initial: 1 mg; may repeat every 3 to 4 hours as needed; usual range: 0.5 to 2 mg every 3 to 4 hours as needed.

Intranasal (spray): Initial: One spray (1 mg per spray) in 1 nostril; if adequate pain relief is not achieved within 60 to 90 minutes, an additional 1 spray in 1 nostril may be given; may repeat initial dose sequence in 3 to 4 hours after the last dose as needed.

Alternatively (depending on severity of pain), an initial dose of 2 mg (1 spray in each nostril) may be used in patients who will be able to remain recumbent (in the event drowsiness or dizziness occurs); additional doses should not be repeated for at least 3 to 4 hours after the initial dose.

Discontinuation of therapy: When reducing the dose, discontinuing, or tapering long-term opioid therapy, the dose should be gradually tapered. An optimal tapering schedule has not been established. Individualize tapering based on discussions with patient to minimize withdrawal, while considering patient-specific goals and concerns and the opioid’s pharmacokinetics. Proposed initial schedules range from slow (eg, 10% reduction per week or 10% reduction per month depending on duration of long-term therapy) to rapid (eg, 25% to 50% reduction every few days) (Ref). Slower tapers may be appropriate after long-term use (eg, >1 year), whereas more rapid tapers may be appropriate in patients experiencing severe adverse effects. During tapering, patients may be at an increased risk of overdose if they return to their original (or higher) opioid dose or use illicit opioids, due to rapid loss of tolerance; consider prescribing naloxone or nalmefene. Monitor carefully for signs/symptoms of withdrawal. If the patient displays withdrawal symptoms, consider slowing the taper schedule; alterations may include increasing the interval between dose reductions, decreasing amount of daily dose reduction, pausing the taper and restarting when the patient is ready, and/or coadministration of an alpha-2 agonist (eg, clonidine) to blunt autonomic withdrawal symptoms and other adjunctive agents to treat GI symptoms and muscle spasms, as needed. Continue to offer nonopioid analgesics as needed for pain management during the taper (Ref).

Pain during labor

Pain during labor (fetus ≥37 weeks' gestation and no signs of fetal distress):

Note: Alternative analgesia should be used for pain associated with delivery or if delivery is anticipated within 4 hours.

IM, IV: 1 to 2 mg; may repeat in 4 hours.

Preoperative sedation

Preoperative sedation:

IV: 2 mg once; administer shortly before induction.

IM: 2 mg once; administer 60 to 90 minutes before surgery.

Supplement to balanced anesthesia

Supplement to balanced anesthesia: IV: 2 mg shortly before induction; may be followed by incremental doses of 0.5 to 1 mg as needed during anesthesia (incremental dose dependent on previously administered sedative, analgesic, and hypnotic medications); usual total dose: 4 to 12.5 mg.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Acute pain (including pain during labor [fetus ≥37 weeks' gestation and no signs of fetal distress]) (alternative agent) :

IM: Initial: 1 mg; repeated dosing must be based on initial response rather than fixed intervals, but generally at least 6 hours from previous dose.

IV: Initial: 0.5 mg; repeated dosing must be based on initial response rather than fixed intervals, but generally at least 6 hours from previous dose.

Intranasal (spray): Initial: One spray (1 mg per spray) in 1 nostril; if adequate pain relief is not achieved within 90 to 120 minutes, an additional 1 spray in 1 nostril may be given. May repeat initial dose sequence as needed at intervals determined by patient response; usual interval: ≥6 hours between dosing sequences.

Preoperative sedation and supplement to balanced anesthesia: There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Liver Impairment: Adult

Acute pain (including pain during labor [fetus ≥37 weeks' gestation and no signs of fetal distress]) (alternative agent) :

IM: Initial: 1 mg; repeated dosing must be based on initial response rather than fixed intervals, but generally at least 6 hours from previous dose.

IV: Initial: 0.5 mg; repeated dosing must be based on initial response rather than fixed intervals, but generally at least 6 hours from previous dose.

Intranasal (spray): Initial: One spray (1 mg per spray) in 1 nostril; if adequate pain relief is not achieved within 90 to 120 minutes, an additional 1 spray in 1 nostril may be given. May repeat initial dose sequence as needed at intervals determined by patient response; usual interval: ≥6 hours between dosing sequences.

Preoperative sedation and supplement to balanced anesthesia: There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Note: Minimize opioid use in older adults unless for the management of severe acute pain. Opioids are associated with an increased risk of falls and inducing or worsening delirium in older adults (Ref).

Acute pain (alternative agent):

IM: Initial: 1 mg; repeated dosing must be based on initial response rather than fixed intervals, but generally at least 6 hours from previous dose.

IV: Initial: 0.5 mg; repeated dosing must be based on initial response rather than fixed intervals, but generally at least 6 hours from previous dose.

Intranasal (spray): Initial: One spray (1 mg per spray) in 1 nostril; if adequate pain relief is not achieved within 90 to 120 minutes, an additional 1 spray in 1 nostril may be given. May repeat initial dose sequence as needed at intervals determined by patient response; usual interval: ≥6 hours between dosing sequences.

Refer to adult dosing for additional uses.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for injection and nasal spray formulations, unless otherwise noted.

>10%:

Gastrointestinal: Nausea and vomiting (8% to 13%)

Nervous system: Dizziness (19% to 23%), drowsiness (43% to 49%), insomnia (nasal spray: 11%)

Respiratory: Nasal congestion (nasal spray: 13%)

1% to 10%:

Cardiovascular: Hypertension (including severe hypertension), hypotension, palpitations, vasodilation

Dermatologic: Diaphoresis, pruritus

Gastrointestinal: Anorexia, constipation, diarrhea (nasal spray), stomach pain, unpleasant taste, xerostomia

Nervous system: Anxiety, asthenia, confusion, euphoria, feeling hot, floating feeling, headache, lethargy, nervousness, paresthesia, tremor

Ophthalmic: Blurred vision

Otic: Otalgia, tinnitus

Respiratory: Cough, dyspnea, epistaxis (nasal spray), nasal discomfort (nasal spray: irritation), paranasal sinus congestion (nasal spray), rhinitis (nasal spray), sinusitis (nasal spray), sore nose (nasal spray)

<1%:

Cardiovascular: Chest pain, edema, syncope, tachycardia

Dermatologic: Skin rash, urticaria

Genitourinary: Urination disorder

Nervous system: Abnormal dreams, agitation, allodynia (opioid-induced hyperalgesia), depression, dysphoria, hallucination, hostility, opioid withdrawal syndrome

Respiratory: Shallow respiration

Frequency not defined:

Nervous system: Drug abuse, neonatal withdrawal, opioid dependence

Respiratory: Respiratory depression

Postmarketing (any formulation):

Genitourinary: Hypogonadism (Brennan 2013; Debono 2011)

Hypersensitivity: Anaphylaxis

Contraindications

Hypersensitivity (eg, anaphylaxis) to butorphanol, benzethonium chloride (preservative), or any component of the formulation; acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment; significant respiratory depression; GI obstruction, including paralytic ileus (known or suspected).

Canadian labeling: Additional contraindications for nasal spray (not in the US labeling): Suspected surgical abdomen (eg, acute appendicitis or pancreatitis); any disease/condition that affects bowel transit (eg, ileus of any type); mild pain manageable with other pain medications; chronic obstructive airway; status asthmaticus; hypercapnia and cor pulmonale; acute alcoholism; delirium tremors; seizure disorder; severe CNS depression; increased cerebrospinal or intracranial pressure; head injury; concomitant use with or within 14 days following monoamine oxidase inhibitor therapy; breastfeeding; pregnancy; use during labor and delivery.

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Hyperalgesia: Opioid-induced hyperalgesia (OIH) has occurred with short-term and prolonged use of opioid analgesics. Symptoms may include increased levels of pain upon opioid dosage increase, decreased levels of pain upon opioid dosage decrease, or pain from ordinarily nonpainful stimuli; symptoms may be suggestive of OIH if there is no evidence of underlying disease progression, opioid tolerance, opioid withdrawal, or addictive behavior. Consider decreasing the current opioid dose or opioid rotation in patients who experience OIH.

• Hypotension: May cause severe hypotension (including orthostatic hypotension and syncope); use with caution in patients with hypovolemia, cardiovascular disease (including acute myocardial infarction [MI]), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics). Monitor for symptoms of hypotension following initiation or dose titration. Use with caution in patients with circulatory shock.

• Phenanthrene hypersensitivity: Use with caution in patients with hypersensitivity reactions to other phenanthrene-derivative opioid agonists (eg, codeine, hydromorphone, levorphanol, oxycodone, oxymorphone).

• Respiratory depression: Fatal respiratory depression may occur. Carbon dioxide retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids. Patients and caregivers should be educated on how to recognize respiratory depression and the importance of getting emergency assistance immediately (eg, calling 911) in the event of known or suspected overdose.

Disease-related concerns:

• Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions.

• Adrenocortical insufficiency: Use with caution in patients with adrenal insufficiency, including Addison disease. Long-term opioid use may cause secondary hypogonadism, which may lead to mood disorders and osteoporosis (Brennan 2013).

• Biliary tract impairment: Use with caution in patients with biliary tract dysfunction, including acute pancreatitis; may cause constriction of sphincter of Oddi.

• Cardiovascular disease: Use extreme caution in patients with acute myocardial infarction, ventricular dysfunction, or coronary insufficiency; limit use to situations where the benefits clearly outweigh the risk.

• CNS depression/coma: Avoid use in patients with impaired consciousness or coma as these patients are susceptible to intracranial effects of CO2 retention.

• Delirium tremens: Use with caution in patients with delirium tremens.

• Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure (ICP); exaggerated elevation of ICP may occur.

• Hepatic impairment: Use with caution in patients with hepatic impairment. Dosage adjustments are recommended.

• Mental health conditions: Use opioids with caution for chronic pain in patients with mental health conditions (eg, depression, anxiety disorders, post-traumatic stress disorder) due to potential increased risk for opioid use disorder and overdose; more frequent monitoring is recommended (CDC [Dowell 2022]).

• Obesity: Use with caution in patients who are morbidly obese.

• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.

• Psychosis: Use with caution in patients with toxic psychosis.

• Renal impairment: Use with caution in patients with renal impairment. Dosage adjustments are recommended.

• Respiratory disease: Use with caution and monitor for respiratory depression in patients with significant chronic obstructive pulmonary disease or cor pulmonale, and those with a substantially decreased respiratory reserve, hypoxia, hypercapnia, or preexisting respiratory depression, particularly when initiating and titrating therapy; critical respiratory depression may occur, even at therapeutic dosages. Consider the use of alternative nonopioid analgesics in these patients.

• Seizures: Use with caution in patients with a history of seizure disorders; may cause or exacerbate preexisting seizures.

• Serotonin syndrome: Potentially life-threatening serotonin syndrome (SS) has occurred with concomitant use of butorphanol and serotonergic agents (eg, selective serotonin reuptake inhibitors, serotonin and norepinephrine reuptake inhibitors, triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, buspirone, St John's wort, tryptophan) or agents that impair metabolism of serotonin (eg, monoamine oxidase [MAO] inhibitors intended to treat psychiatric disorders, other MAO inhibitors [ie, linezolid and intravenous methylene blue]). Monitor patients closely for signs of SS such as mental status changes (eg, agitation, hallucinations, delirium, coma); autonomic instability (eg, tachycardia, labile blood pressure, diaphoresis); neuromuscular changes (eg, tremor, rigidity, myoclonus); GI symptoms (eg, nausea, vomiting, diarrhea); and/or seizures.

• Sleep-related disorders: Use with caution in patients with sleep-related disorders, including sleep apnea, due to increased risk for respiratory and central nervous system depression. Monitor carefully and titrate dosage cautiously in patients with mild sleep-disordered breathing. Avoid opioids in patients with moderate to severe sleep-disordered breathing (CDC [Dowell 2022]).

• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.

Concurrent drug therapy issues:

• Benzodiazepines or other CNS depressants (intranasal): Concomitant use may result in respiratory depression and sedation, which may be fatal. Consider prescribing naloxone or nalmefene for emergency treatment of opioid overdose in patients taking benzodiazepines or other CNS depressants concomitantly with opioids.

Special populations:

• Cachectic or debilitated patients: Use with caution in cachectic or debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages. Consider the use of alternative nonopioid analgesics in these patients.

• Older adults: Use opioids with caution in older adults; may be more sensitive to adverse effects. Clearance may also be reduced in older adults (with or without renal impairment) resulting in a narrow therapeutic window and increased adverse effects. Monitor closely for adverse effects associated with opioid therapy (eg, respiratory and central nervous system depression, falls, cognitive impairment, constipation) (CDC [Dowell 2022]). Consider the use of alternative nonopioid analgesics in these patients when possible.

• Neonates: Neonatal opioid withdrawal syndrome: Signs and symptoms include irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and failure to gain weight. Onset, duration, and severity depend on the drug used, duration of use, maternal dose, and rate of drug elimination by the newborn.

Other warnings/precaution:

• Abrupt discontinuation/withdrawal: Abrupt discontinuation in patients who are physically dependent to opioids has been associated with serious withdrawal symptoms, uncontrolled pain, attempts to find other opioids (including illicit), and suicide. Use a collaborative, patient-specific taper schedule that minimizes the risk of withdrawal, considering factors such as current opioid dose, duration of use, type of pain, and physical and psychological factors. Monitor pain control, withdrawal symptoms, mood changes, suicidal ideation, and for use of other substances and provide care as needed. Concurrent use of agonist/partial agonist or agonist/antagonist analgesics may also precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists.

• Abuse/misuse/diversion: Use with caution in patients with a history of substance abuse disorder; potential for drug dependency exists. Other factors associated with increased risk for misuse include concomitant depression or other mental health conditions, higher opioid dosages, or taking other central nervous system depressants. Consider offering naloxone or nalmefene prescriptions in patients with an increased risk for overdose, such as history of overdose or substance use disorder, higher opioid dosages (≥50 morphine milligram equivalents [MME]/day orally), concomitant benzodiazepine use, and patients at risk for returning to a high dose after losing tolerance (CDC [Dowell 2022]).

• Appropriate use: Outpatient setting: Opioids should not be used as first-line therapy for acute (<1-month duration), subacute (1- to 3-month duration), or chronic pain (>3-month duration [outside of end-of-life or palliative care, active cancer treatment, sickle cell disease, or medication-based opioid use disorder treatment]). Preferred management includes nonpharmacologic therapy and nonopioid therapy (eg, nonsteroidal anti-inflammatory drugs, acetaminophen, certain antiseizure medications and antidepressants) as appropriate for the specific condition. If opioid therapy is initiated, it should be combined with nonpharmacologic and non-opioid therapy, as appropriate. Prior to initiation, known risks and realistic benefits of opioid therapy should be discussed with the patient. Therapy should be initiated at the lowest effective dosage using IR opioids (instead of ER/long-acting opioids). For the treatment of acute pain, therapy should only be given for the expected duration of pain severe enough to require opioids and prescribed as needed (not scheduled). For the treatment of subacute and chronic pain, realistic treatment goals for pain/function should be established, including consideration for discontinuation if benefits do not outweigh risks. Therapy should be continued only if clinically meaningful improvement in pain/function outweighs risks. Risk to patients increases with higher opioid dosages. Dosages ≥50 MME/day are likely to not have increased benefit to pain relief or function relative to overall risk to patients; before increasing dosage to ≥50 MME/day, readdress pain and reassess evidence of individual benefits and risks (CDC [Dowell 2022]).

• Naloxone/Nalmefene access: Discuss the availability of naloxone or nalmefene with all patients who are prescribed opioid analgesics, as well as their caregivers, and consider prescribing it to patients who are at increased risk of opioid overdose. These include patients who are also taking benzodiazepines or other CNS depressants, have an opioid use disorder (OUD) (current or history of), or have experienced opioid-induced respiratory depression/opioid overdose. Additionally, health care providers should consider prescribing naloxone or nalmefene to patients prescribed medications to treat OUD; patients at risk of opioid overdose even if they are not taking an opioid analgesic or medication to treat OUD; and patients taking opioids, including methadone or buprenorphine for OUD, if they have household members, including children, or other close contacts at risk for accidental ingestion or opioid overdose. Inform patients and caregivers on options for obtaining naloxone or nalmefene (eg, by prescription, directly from a pharmacist, a community-based program) as permitted by state dispensing and prescribing guidelines. Educate patients and caregivers on how to recognize respiratory depression, proper administration of naloxone or nalmefene, and getting emergency help.

• Optimal regimen: An opioid-containing analgesic regimen should be tailored to each patient's needs and based upon the type of pain being treated (acute versus chronic), the route of administration, degree of tolerance for opioids (naive versus chronic user), age, weight, and medical condition. The optimal analgesic dose varies widely among patients; doses should be titrated to pain relief/prevention.

• Surgery: Opioids decrease bowel motility; monitor for decrease bowel motility in postoperative patients receiving opioids.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection, as tartrate:

Generic: 2 mg/mL (1 mL, 2 mL)

Solution, Injection, as tartrate [preservative free]:

Generic: 1 mg/mL (1 mL)

Solution, Nasal, as tartrate:

Generic: 10 mg/mL (2.5 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Butorphanol Tartrate Injection)

1 mg/mL (per mL): $9.79

2 mg/mL (per mL): $11.98

Solution (Butorphanol Tartrate Nasal)

10 mg/mL (per mL): $38.53

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Nasal, as tartrate:

Generic: 10 mg/mL (2.5 mL)

Controlled Substance

C-IV

Administration: Adult

IV: Administer IV.

IM: Administer IM.

Intranasal: Fully prime pump prior to initial use; pump spray firmly and quickly until a fine mist appears (up to 7 to 8 strokes). If not used for ≥48 hours, reprime with 1 or 2 strokes. Aim spray away from self and others when priming. Gently blow nose to clear nasal passages; insert spray ~1 centimeter into nostril pointing tip to the back of the nose; tilt head slightly forward and close one nostril gently with index finger; pump spray firmly and quickly by pushing down on finger grips of the pump; gently sniff with mouth closed; remove pump and tilt head backwards gently sniffing for a few more seconds. If a 2-spray dose is needed, administer second spray in the other nostril (follow steps above).

Use: Labeled Indications

Acute pain: Management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Limitations of use: Because of the risks of substance use disorder, abuse, and misuse with opioids, which may occur at any dosage or duration, reserve butorphanol for use in patients for whom alternative treatment options (eg, nonopioid analgesics) have not been tolerated or are not expected to be tolerated; have not provided adequate analgesia or are not expected to provide adequate analgesia. Not intended to be used for an extended period of time unless the pain remains severe enough to require an opioid analgesic and for which alternative treatment options continue to be inadequate.

Pain during labor (fetus ≥37 weeks' gestation and no signs of fetal distress) (injection only): Management of pain during labor.

Limitations of use: Because of the risks of substance use disorder, abuse, and misuse with opioids, which may occur at any dosage or duration, reserve butorphanol for use in patients for whom alternative treatment options (eg, nonopioid analgesics) have not been tolerated or are not expected to be tolerated; have not provided adequate analgesia or are not expected to provide adequate analgesia. Not intended to be used for an extended period of time unless the pain remains severe enough to require an opioid analgesic and for which alternative treatment options continue to be inadequate.

Preoperative sedation (injection only): Preoperative or preanesthetic medication.

Supplement to balanced anesthesia (injection only): Supplement to balanced anesthesia.

Medication Safety Issues
Sound-alike/look-alike issues:

Stadol may be confused with Haldol, sotalol

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (opioids, all formulations and routes of administration) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).

Metabolism/Transport Effects

Substrate of CYP3A4 (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Agents with Clinically Relevant Anticholinergic Effects: May increase adverse/toxic effects of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor

Alizapride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Alvimopan: Opioid Agonists may increase adverse/toxic effects of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Risk D: Consider Therapy Modification

Amisulpride (Oral): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Amphetamines: May increase analgesic effects of Opioid Agonists. Risk C: Monitor

Articaine: May increase CNS depressant effects of CNS Depressants. Management: Consider reducing the dose of articaine if possible when used in patients who are also receiving CNS depressants. Monitor for excessive CNS depressant effects with any combined use. Risk D: Consider Therapy Modification

Azelastine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Benperidol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Blonanserin: CNS Depressants may increase CNS depressant effects of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider Therapy Modification

Brimonidine (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromopride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromperidol: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Buclizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Buprenorphine: Opioids (Mixed Agonist / Antagonist) may decrease therapeutic effects of Buprenorphine. This combination may also induce opioid withdrawal. Risk X: Avoid

BusPIRone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Cannabinoid-Containing Products: CNS Depressants may increase CNS depressant effects of Cannabinoid-Containing Products. Risk C: Monitor

Cetirizine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk D: Consider Therapy Modification

Chloral Hydrate/Chloral Betaine: CNS Depressants may increase CNS depressant effects of Chloral Hydrate/Chloral Betaine. Management: Consider alternatives to the use of chloral hydrate or chloral betaine and additional CNS depressants. If combined, consider a dose reduction of either agent and monitor closely for enhanced CNS depressive effects. Risk D: Consider Therapy Modification

Chlormethiazole: May increase CNS depressant effects of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider Therapy Modification

Chlorphenesin Carbamate: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

CNS Depressants: May increase CNS depressant effects of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

CYP3A4 Inducers (Strong): May decrease serum concentration of Butorphanol. Risk C: Monitor

CYP3A4 Inhibitors (Strong): May increase serum concentration of Butorphanol. Risk C: Monitor

Daridorexant: May increase CNS depressant effects of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification

Desmopressin: Opioid Agonists may increase hyponatremic effects of Desmopressin. Risk C: Monitor

DexmedeTOMIDine: CNS Depressants may increase CNS depressant effects of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider Therapy Modification

Difelikefalin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dihydralazine: CNS Depressants may increase hypotensive effects of Dihydralazine. Risk C: Monitor

Dimethindene (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Diuretics: Opioid Agonists may increase adverse/toxic effects of Diuretics. Opioid Agonists may decrease therapeutic effects of Diuretics. Risk C: Monitor

Dothiepin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

DroPERidol: May increase CNS depressant effects of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider Therapy Modification

Eluxadoline: Opioid Agonists may increase constipating effects of Eluxadoline. Risk X: Avoid

Emedastine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk C: Monitor

Entacapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Flunarizine: CNS Depressants may increase CNS depressant effects of Flunarizine. Risk X: Avoid

Flunitrazepam: CNS Depressants may increase CNS depressant effects of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider Therapy Modification

Gastrointestinal Agents (Prokinetic): Opioid Agonists may decrease therapeutic effects of Gastrointestinal Agents (Prokinetic). Risk C: Monitor

HydrOXYzine: May increase CNS depressant effects of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider Therapy Modification

Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies): May decrease therapeutic effects of Opioid Agonists. Opioid Agonists may decrease therapeutic effects of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor

Ixabepilone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kava Kava: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ketotifen (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kratom: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Lemborexant: May increase CNS depressant effects of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider Therapy Modification

Levocetirizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Levomethadone: Opioids (Mixed Agonist / Antagonist) may decrease analgesic effects of Levomethadone. Risk X: Avoid

Lisuride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lofexidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Loxapine: CNS Depressants may increase CNS depressant effects of Loxapine. Management: Consider reducing the dose of CNS depressants administered concomitantly with loxapine due to an increased risk of respiratory depression, sedation, hypotension, and syncope. Risk D: Consider Therapy Modification

Magnesium Sulfate: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Mequitazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metergoline: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Methotrimeprazine: CNS Depressants may increase CNS depressant effects of Methotrimeprazine. Methotrimeprazine may increase CNS depressant effects of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider Therapy Modification

Metoclopramide: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

MetyroSINE: CNS Depressants may increase sedative effects of MetyroSINE. Risk C: Monitor

Minocycline (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Monoamine Oxidase Inhibitors: Butorphanol may increase serotonergic effects of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Risk X: Avoid

Moxonidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Nabilone: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Nalfurafine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Nalfurafine: Opioid Agonists may increase adverse/toxic effects of Nalfurafine. Opioid Agonists may decrease therapeutic effects of Nalfurafine. Risk C: Monitor

Nalmefene: May decrease therapeutic effects of Opioid Agonists. Management: Avoid the concomitant use of oral nalmefene and opioid agonists. Discontinue oral nalmefene 1 week prior to any anticipated use of opioid agonists. If combined, larger doses of opioid agonists will likely be required. Risk D: Consider Therapy Modification

Naltrexone: May decrease therapeutic effects of Opioid Agonists. Management: Seek therapeutic alternatives to opioids. See full drug interaction monograph for detailed recommendations. Risk X: Avoid

Noscapine: CNS Depressants may increase adverse/toxic effects of Noscapine. Risk X: Avoid

Olopatadine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Opicapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Opioid Agonists: CNS Depressants may increase CNS depressant effects of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

Opioid Agonists: Opioids (Mixed Agonist / Antagonist) may decrease analgesic effects of Opioid Agonists. Management: Seek alternatives to mixed agonist/antagonist opioids in patients receiving pure opioid agonists, and monitor for symptoms of therapeutic failure/high dose requirements (or withdrawal in opioid-dependent patients) if patients receive these combinations. Risk X: Avoid

Opipramol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Orphenadrine: CNS Depressants may increase CNS depressant effects of Orphenadrine. Risk X: Avoid

Oxomemazine: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Oxybate Salt Products: CNS Depressants may increase CNS depressant effects of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider Therapy Modification

Paraldehyde: CNS Depressants may increase CNS depressant effects of Paraldehyde. Risk X: Avoid

Pegvisomant: Opioid Agonists may decrease therapeutic effects of Pegvisomant. Risk C: Monitor

Periciazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Pipamperone: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

Piribedil: CNS Depressants may increase CNS depressant effects of Piribedil. Risk C: Monitor

Pramipexole: CNS Depressants may increase sedative effects of Pramipexole. Risk C: Monitor

Procarbazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ramosetron: Opioid Agonists may increase constipating effects of Ramosetron. Risk C: Monitor

Rilmenidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ropeginterferon Alfa-2b: CNS Depressants may increase adverse/toxic effects of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider Therapy Modification

ROPINIRole: CNS Depressants may increase sedative effects of ROPINIRole. Risk C: Monitor

Rotigotine: CNS Depressants may increase sedative effects of Rotigotine. Risk C: Monitor

Samidorphan: May decrease therapeutic effects of Opioid Agonists. Risk X: Avoid

Serotonergic Agents (High Risk): Opioid Agonists may increase serotonergic effects of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor

Sincalide: Drugs that Affect Gallbladder Function may decrease therapeutic effects of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Risk D: Consider Therapy Modification

Somatostatin Analogs: Opioid Agonists may decrease analgesic effects of Somatostatin Analogs. Opioid Agonists may increase analgesic effects of Somatostatin Analogs. Risk C: Monitor

Succinylcholine: May increase bradycardic effects of Opioid Agonists. Risk C: Monitor

Suvorexant: CNS Depressants may increase CNS depressant effects of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification

Thalidomide: CNS Depressants may increase CNS depressant effects of Thalidomide. Risk X: Avoid

Tilidine: May increase therapeutic effects of Opioid Agonists. Risk X: Avoid

Valerian: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Zolpidem: CNS Depressants may increase CNS depressant effects of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider Therapy Modification

Zuranolone: May increase CNS depressant effects of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider Therapy Modification

Reproductive Considerations

Chronic opioid use may cause hypogonadism and hyperprolactinemia, which may decrease fertility in patients of reproductive potential. Menstrual cycle disorders (including amenorrhea), erectile dysfunction, and impotence have been reported. The incidence of hypogonadism may be increased with the use of opioids in high doses or long-acting opioid formulations. It is not known if the effects on fertility are reversible. Monitor patients on long-term therapy (de Vries 2020; Gadelha 2022).

Consider family planning, contraception, and the effects on fertility prior to prescribing opioids for chronic pain to patients who could become pregnant (ACOG 2017; CDC [Dowell 2022]).

Pregnancy Considerations

Butorphanol crosses the placenta

Butorphanol can be detected in neonatal serum following maternal IM injection prior to delivery (Pittman 1980).

Maternal use of opioids may be associated with poor fetal growth, stillbirth, and preterm delivery (CDC [Dowell 2022]). Opioids used as part of obstetric analgesia/anesthesia during labor and delivery may temporarily affect the fetal heart rate (ACOG 2019).

Neonatal abstinence syndrome (NAS)/neonatal opioid withdrawal syndrome (NOWS) may occur following prolonged in utero exposure to opioids (CDC [Dowell 2022]). NAS/NOWS may be life-threatening if not recognized and treated and requires management according to protocols developed by neonatology experts. Presentation of symptoms varies by opioid characteristics (eg, immediate release, sustained release), time of last dose prior to delivery, drug metabolism (maternal, placental, and infant), net placental transfer, as well as other factors (AAP [Hudak 2012]; AAP [Patrick 2020]). Clinical signs characteristic of withdrawal following in utero opioid exposure include excessive crying or easily irritable, fragmented sleep (<2 to 3 hours after feeding), tremors, increased muscle tone, or GI dysfunction (hyperphagia, poor feeding, feeding intolerance, watery or loose stools) (Jilani 2022). NAS/NOWS occurs following chronic opioid exposure and would not be expected following the use of opioids at delivery (AAP [Patrick 2020]).

Monitor infants of mothers on long-term/chronic opioid therapy for symptoms of withdrawal. Symptom onset reflects the half-life of the opioid used. Monitor infants for at least 3 days following exposure to immediate-release opioids; monitor for at least 4 to 7 days following exposure to sustained-release opioids (AAP [Patrick 2020]; CDC [Dowell 2022]). Monitor newborns for excess sedation and respiratory depression when opioids are used during labor.

When opioids are needed to treat acute pain in pregnant patients, the lowest effective dose for only the expected duration of pain should be prescribed (CDC [Dowell 2022]).

Butorphanol injection is approved for preoperative or preanesthetic medication and as a supplement to balanced anesthesia. The ACOG recommends that pregnant patients should not be denied medically necessary surgery, regardless of trimester. If the procedure is elective, it should be delayed until after delivery (ACOG 2019).

Butorphanol injection is approved for the management of pain during labor; apnea or respiratory distress in the newborn may occur. The manufacturer recommends that caution be used if abnormal fetal heart rate patterns are present.

Opioid use for pain following vaginal or cesarean delivery should be made as part of a shared decision-making process. A stepwise multimodal approach to managing postpartum pain is recommended. A low-dose, low-potency, short-acting opioid can be used to treat acute pain associated with delivery when needed (ACOG 2021).

Opioids are not preferred for the treatment of chronic noncancer pain during pregnancy; consider strategies to minimize or avoid opioid use. Advise pregnant patients requiring long-term opioid use of the risk of NAS/NOWS and provide appropriate treatment for the neonate after delivery. NAS/NOWS is an expected and treatable condition following chronic opioid use during pregnancy and should not be the only reason to avoid treating pain with an opioid in pregnant patients (ACOG 2017; CDC [Dowell 2022]). Do not abruptly discontinue opioids during pregnancy; taper prior to discontinuation when appropriate, considering the risks to the pregnant patient and fetus if maternal withdrawal occurs (CDC [Dowell 2022]).

Breastfeeding Considerations

Butorphanol is present in breast milk.

Butorphanol concentrations in breast milk were evaluated in six women following a single maternal dose of 2 mg IM administered 79 ± 20 hours after delivery. The highest concentrations appeared 1 hour after the dose (1.5 ± 0.9 ng/mL) and decreased to 0.3 ± 0.2 ng/mL 6 hours after the dose (Pittman 1980).

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Nonopioid analgesics are preferred for lactating patients who require pain control peripartum or for surgery outside of the postpartum period. When opioids are needed for lactating patients, use the lowest effective dose for the shortest duration of time to limit adverse events in the mother and breastfeeding infant. Use of butorphanol may be considered when an opioid is needed (AAP [Sachs 2013]; ABM [Martin 2018]; ABM [Reece-Stremtan 2017]; WHO 2002).

When chronic opioids are prescribed prenatally and continued postpartum, breastfeeding may be initiated to help mitigate potential newborn withdrawal; monitor both the mother and the infant (AAP [Meek 2022]; AAP [Patrick 2020]).

Monitor infants exposed to opioids via breast milk for drowsiness, sedation, feeding difficulties, or limpness (ACOG 2019). Withdrawal symptoms may occur when maternal use is discontinued, or breastfeeding is stopped.

The Academy of Breastfeeding Medicine recommends postponing elective surgery until milk supply and breastfeeding are established. Milk should be expressed ahead of surgery when possible. In general, when the child is healthy and full term, breastfeeding may resume, or milk may be expressed once the mother is awake and in recovery. For children who are at risk for apnea, hypotension, or hypotonia, milk may be saved for later use when the child is at lower risk (ABM [Reece-Stremtan 2017]).

Monitoring Parameters

Pain relief, respiratory and mental status, BP; bowel function; signs/symptoms of substance use disorder, abuse, or misuse; signs or symptoms of hypogonadism or hypoadrenalism (Brennan 2013).

Alternate recommendations: Subacute or chronic pain (long-term therapy outside of end-of-life or palliative care, active cancer treatment, sickle cell disease, or medication-based opioid use disorder treatment): Evaluate benefits/risks of opioid therapy within 1 to 4 weeks of treatment initiation and with dose increases. In patients with subacute pain initially treated for acute pain, reassess pain and function after 30 days to address potentially reversible causes of pain and prevent unintentional long-term opioid therapy. In patients on long-term therapy, re-evaluate benefits/risks every 3 months during therapy or more frequently in patients at increased risk of overdose or opioid use disorder. Toxicology testing is recommended prior to initiation and at least yearly (includes controlled prescription medications, illicit drugs of abuse, and benzodiazepines). State prescription drug monitoring program (PDMP) data should be reviewed by clinicians prior to initiation and periodically during therapy (frequency ranging from every prescription to every 3 months) (CDC [Dowell 2022]).

Reference Range

0.7 to 1.5 ng/mL

Mechanism of Action

Agonist of kappa opiate receptors and partial agonist of mu opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces analgesia, respiratory depression, and sedation similar to opioids

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: IM, nasal: ≤15 minutes; IV: Within a few minutes.

Peak effect: IM, IV: 0.5 to 1 hour; Nasal: 1 to 2 hours.

Duration: IM, IV: 3 to 4 hours; Nasal: 4 to 5 hours.

Absorption: Rapid and well absorbed.

Distribution: Vd: 305 to 901 L.

Protein binding: ~80%.

Metabolism: Hepatic to major metabolite, hydroxybutorphanol.

Bioavailability: Nasal: 60% to 70%.

Half-life elimination: IV, nasal: ~2 to 9 hours; Hydroxybutorphanol: ~18 hours.

Elderly: IV, nasal: ~3 to 9 hours.

Renal impairment (CrCl <30 mL/minute): ~10.5 hours.

Hepatic impairment: ~16.8 hours.

Time to peak, plasma: IM: 20 to 40 minutes; Nasal: 30 to 60 minutes.

Excretion: Primarily urine (70% to 80%; ~5% unchanged); feces (~15%).

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Altered kidney function: Elimination half-life is approximately doubled and the total body clearance is approximately one-half in patients with CrCl <30 mL/minute.

Hepatic function impairment: Elimination half-life is approximately tripled and total body clearance is approximately one-half. Exposure to butorphanol is significantly greater (about 2-fold).

Older adult: Elimination half-life is increased. Absolute bioavailability of nasal spray is less in elderly women (48%) than in elderly men (75%).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (LT) Lithuania: Moradol;
  • (LV) Latvia: Moradol;
  • (RU) Russian Federation: Moradol
  1. 2023 American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2023 updated AGS Beers Criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2023;71(7):2052-2081. doi:10.1111/jgs.18372 [PubMed 37139824]
  2. American College of Obstetricians and Gynecologists (ACOG). ACOG committee opinion no. 775: nonobstetric surgery during pregnancy. Obstet Gynecol. 2019;133(4):e285-e286. [PubMed 30913200]
  3. American College of Obstetricians and Gynecologists (ACOG). ACOG practice bulletin no. 209: obstetric analgesia and anesthesia. Obstet Gynecol. 2019;133(3):e208-e225. [PubMed 30801474]
  4. American College of Obstetricians and Gynecologists (ACOG) Committee on Clinical Consensus–Obstetrics. Pharmacologic stepwise multimodal approach for postpartum pain management: ACOG clinical consensus no. 1. Obstet Gynecol. 2021;138(3):507-517. doi:10.1097/AOG.0000000000004517 [PubMed 34412076]
  5. American College of Obstetricians and Gynecologists (ACOG) Committee on Clinical Consensus–Obstetrics. Committee opinion no. 711: opioid use and opioid use disorder in pregnancy. Obstet Gynecol. 2017;130(2):e81-e94. doi:10.1097/AOG.0000000000002235 [PubMed 28742676]
  6. Brennan MJ. The effect of opioid therapy on endocrine function. Am J Med. 2013;126(3)(suppl 1):S12-S18. doi: 10.1016/j.amjmed.2012.12.001. [PubMed 23414717]
  7. Butorphanol tartrate injection [prescribing information]. Lake Forest, IL: Hospira Inc; January 2024.
  8. Butorphanol tartrate nasal solution [prescribing information]. Eatontown, NJ: West-Ward Pharmaceuticals Corp; August 2018.
  9. Butorphanol tartrate nasal spray [prescribing information]. Weston, FL: Apotex Corp; January 2024.
  10. Butorphanol tartrate nasal spray [prescribing information]. Weston, FL: Apotex Corp; September 2023.
  11. Butorphanol tartrate nasal spray [product monograph]. Vaughan, Ontario, Canada: AA Pharma Inc; January 2023.
  12. Centers for Disease Control and Prevention (CDC). Common elements in guidelines for prescribing opioids for chronic pain. https://www.cdc.gov/drugoverdose/pdf/common_elements_in_guidelines_for_prescribing_opioids-a.pdf. Published 2015. Accessed September 13, 2018.
  13. Chou R, Gordon DB, de Leon-Casasola OA, et al. Management of postoperative pain: a clinical practice guideline from the American Pain Society, the American Society of Regional Anesthesia and Pain Medicine, and the American Society of Anesthesiologists' committee on regional anesthesia, executive committee, and administrative council. J Pain. 2016;17(2):131-157. doi:10.1016/j.jpain.2015.12.008 [PubMed 26827847]
  14. Debono M, Chan S, Rolfe C, Jones TH. Tramadol-induced adrenal insufficiency. Eur J Clin Pharmacol. 2011;67(8):865-867. [PubMed 21243342]
  15. de Vries F, Bruin M, Lobatto DJ, et al. Opioids and their endocrine effects: a systematic review and meta-analysis. J Clin Endocrinol Metab. 2020;105(3):1020–1029. doi:10.1210/clinem/dgz022 [PubMed 31511863]
  16. Dowell D, Ragan KR, Jones CM, Baldwin GT, Chou R. CDC clinical practice guideline for prescribing opioids for pain - United States, 2022. MMWR Recomm Rep. 2022;71(3):1-95. doi:10.15585/mmwr.rr7103a1 [PubMed 36327391]
  17. Gadelha MR, Karavitaki N, Fudin J, Bettinger JJ, Raff H, Ben-Shlomo A. Opioids and pituitary function: expert opinion. Pituitary. 2022;25(1):52-63. doi:10.1007/s11102-021-01202-y [PubMed 35066756]
  18. Gaver RC, Vasiljev M, Wong H, et al, “Disposition of Parenteral Butorphanol in Man,” Drug Metab Dispos, 1980, 8(4):230-5. [PubMed 6105056]
  19. Hill MV, Stucke RS, McMahon ML, Beeman JL, Barth RJ Jr. An educational intervention decreases opioid prescribing after general surgical operations. Ann Surg. 2018;267(3):468-472. doi:10.1097/SLA.0000000000002198 [PubMed 28267689]
  20. Hoskin PJ, Hanks GW. Opioid agonists-antagonist drugs in acute and chronic pain states. Drugs. 1991;41(3):326-344. doi:10.2165/00003495-199141030-00002 [PubMed 1711441]
  21. Hudak ML, Tan RC; Committee on Drugs. Neonatal drug withdrawal. Pediatrics. 2012;129(2):e540-e560. [PubMed 22291123]
  22. Jilani SM, Jones HE, Grossman M, et al. Standardizing the clinical definition of opioid withdrawal in the neonate. J Pediatr. 2022;243:33-39.e1. doi:10.1016/j.jpeds.2021.12.021 [PubMed 34942181]
  23. Martin E, Vickers B, Landau R, Reece-Stremtan S. ABM clinical protocol #28, peripartum analgesia and anesthesia for the breastfeeding mother. Breastfeed Med. 2018;13(3):164-171. [PubMed 29595994]
  24. Meek JY, Noble L; Section on Breastfeeding. Policy statement: breastfeeding and the use of human milk. Pediatrics. 2022;150(1):e2022057988. doi:10.1542/peds.2022-057988 [PubMed 35921640]
  25. Patrick SW, Barfield WD, Poindexter BB; Committee on Fetus and Newborn, Committee on Substance Use and Prevention. Neonatal opioid withdrawal syndrome. Pediatrics. 2020;146(5):e2020029074. doi:10.1542/peds.2020-029074 [PubMed 33106341]
  26. Pittman KA, Smyth RD, Losada M, Zighelboim I, Maduska AL, Sunshine A. Human perinatal distribution of butorphanol. Am J Obstet Gynecol. 1980;138(7 Pt 1):797-800. [PubMed 7446613]
  27. Reece-Stremtan S, Campos M, Kokajko L; Academy of Breastfeeding Medicine. ABM clinical protocol #15: analgesia and anesthesia for the breastfeeding mother, revised 2017. Breastfeed Med. 2017;12(9):500-506. [PubMed 29624435]
  28. Refer to manufacturer's labeling.
  29. Sachs HC; Committee on Drugs. The transfer of drugs and therapeutics into human breast milk: an update on selected topics. Pediatrics. 2013;132(3):e796-e809. [PubMed 23979084]
  30. US Department of Health and Human Services. HHS guide for clinicians on the appropriate dosage reduction or discontinuation of long-term opioid analgesics. October 2019. https://www.hhs.gov/opioids/sites/default/files/2019-10/Dosage_Reduction_Discontinuation.pdf.
  31. US Food and Drug Administration (FDA). FDA drug safety communication: FDA updates prescribing information for all opioid pain medicines to provide additional guidance for safe use. https://www.fda.gov/drugs/drug-safety-and-availability/fda-updates-prescribing-information-all-opioid-pain-medicines-provide-additional-guidance-safe-use. Published April 13, 2023. Accessed April 17, 2023.
  32. US Food and Drug Administration (FDA). Postmarket drug safety information for patients and providers: information about naloxone and nalmefene. https://www.fda.gov/drugs/postmarket-drug-safety-information-patients-and-providers/information-about-naloxone-and-nalmefene. Published April 22, 2024. Accessed August 7, 2024.
  33. World Health Organization (WHO). Breastfeeding and maternal medication, recommendations for drugs in the eleventh WHO model list of essential drugs. https://apps.who.int/iris/handle/10665/62435. Published 2002.
Topic 9179 Version 365.0